Characterization of CGS 8515 as a selective 5-lipoxygenase (5-LO) inhibitor

1. CGS 8515 selectively inhibited 5-LO (IC50 = 0.1 microM) with negligible effect on CO, 12-LO, 15-LO and TxS at concentrations up to 100 microM. 2. CGS 8515 selectively inhibited A23187-induced formation of 5-LO products in rat and human whole blood with a 20-70 fold separation of effects over the...

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Bibliographic Details
Published in:	Advances in prostaglandin, thromboxane, and leukotriene research Vol. 19; p. 86
Main Authors:	Ku, E C, Raychaudhuri, A, Ghai, G, Kimble, E F, Lee, W H, Colombo, C, Dotson, R, White, D, Oglesby, T D, Wasley, J W
Format:	Journal Article
Language:	English
Published:	United States 1989
Subjects:	Animals Arachidonate 5-Lipoxygenase - blood Arachidonate Lipoxygenases - blood Arachidonic Acids - blood Calcimycin - pharmacology Cell Movement Humans Kinetics Leukocytes - drug effects Leukocytes - enzymology Leukocytes - physiology Lipoxygenase Inhibitors Naphthoquinones - pharmacology ortho-Aminobenzoates - pharmacology Rats
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Summary:	1. CGS 8515 selectively inhibited 5-LO (IC50 = 0.1 microM) with negligible effect on CO, 12-LO, 15-LO and TxS at concentrations up to 100 microM. 2. CGS 8515 selectively inhibited A23187-induced formation of 5-LO products in rat and human whole blood with a 20-70 fold separation of effects over the formation of CO products. 3. Ex vivo and in vivo studies with rats showed that CGS 8515, at an oral dose of 2-50 mg/kg, significantly inhibited A23187-induced formation of LTs in whole blood and in the lung. The effect persisted for at least 6 h in the ex vivo blood model. 4. CGS 8515, at oral doses as low as 5 mg/kg, significantly suppressed exudate volume and leukocyte migration in the carrageenan-induced pleurisy and sponge models in the rat.
ISSN:	0732-8141